首页工具

购物车

Leniolisib

产品编号 T5166 CAS 1354690-24-6

别名: CDZ173

Leniolisib (CDZ173) 是一种高效的，选择性的 PI3Kδ抑制剂，有用于免疫缺陷类疾病的研究潜力。

TargetMol的所有产品和服务仅用于科学研究，不能被用于人体，我们也不向个人提供产品和服务。

Leniolisib, CAS 1354690-24-6

规格	价格/CNY	货期
1 mg	￥ 627	现货
5 mg	￥ 1,470	现货
10 mg	￥ 2,390	现货
25 mg	￥ 3,970	现货
50 mg	￥ 5,780	现货
100 mg	￥ 7,870	现货
1 mL * 10 mM (in DMSO)	￥ 1,480	现货

大包装超大折扣，点击咨询

其他形式的 Leniolisib:

Leniolisib phosphate
询价

选择批次

纯度: 99.97%

更多批次查询请联系客服

生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Leniolisib (CDZ173) (CDZ173) is a potent and selective PI3Kδ inhibitor (IC50: 11 nM).
靶点活性	PI3Kα:280 nM (cell free), DNA-PK:880 nM (cell free), PI3Kβ:480 nM (cell free), PI3Kδ:11 nM (cell free)
体外活性	Leniolisib (CDZ173) inhibits a large spectrum of immune cell functions, as demonstrated in B and T cells, neutrophils, monocytes, basophils, plasmocytoid dendritic cells, and mast cells [1]. Treatment with CDZ173 caused dose-dependent suppression of PI3Kδ pathway hyperactivation (measured as phosphorylation of AKT/S6) in cell lines ectopically expressing APDS-causative p110δ variants and in T-cell blasts derived from patients [2].
体内活性	In vivo, CDZ173 inhibits B cell activation in rats and monkeys in a concentration- and time-dependent manner. After prophylactic or therapeutic dosing, CDZ173 potently inhibited antigen-specific antibody production and reduced disease symptoms in a rat collagen-induced arthritis model [1]. Oral leniolisib led to a dose-dependent reduction in PI3K/AKT pathway activity assessed ex vivo and improved immune dysregulation. After 12 weeks of treatment, all patients showed amelioration of lymphoproliferation with lymph node sizes and spleen volumes reduced by 39% and 40%, respectively [2].
细胞实验	Studies in transfected Rat-1 fibroblasts and in primary immune cells isolated from patients with APDS were done to assess the in vitro potency of leniolisib on endogenously activated PI3Kδ. PIK3CD mutants encoding published forms of p110δ variants were generated by site-directed mutagenesis using human PIK3CD complementary DNA and transiently transfected in mammalian Rat-1 fibroblasts. The effects of leniolisib and mTOR inhibition on endogenous PI3K/AKT pathway activity in the transfectants were evaluated by measuring phosphorylated AKT (pAKT; S473) using homogeneous time-resolved fluorescence. T-cell blasts from healthy donors as well as APDS patients were generated from isolated T cells by stimulation with anti-CD3 and anti-CD28 antibodies for 3 days. Cells were then incubated with titrated amounts of leniolisib, stimulated with anti-CD3, and the phosphorylation of AKT(S473) and S6(S240/244) was determined by flow cytometry [2].
动物实验	Female wild-type Sprague Dawley rats were kept in standard cages and conditions according to Swiss Animal Welfare guidelines (12h light/dark cycles, RT at 22-24 °C, humidity at least 45 % but <70 %) with free access to Ringer solution (glucose 5%, NaCl 0.9% and KCl 0.5%) and pelleted rodent chow. 96-120 hours before administration of the test substance the animals were anesthetized with isoflurane and catheters were surgically implanted under aseptic precautions (use of sterile instruments and surgical material in combination with local antibiotic prophylaxis) into the femoral artery and vein. The catheters were exteriorized in the neck region, connected to a Harvard swivel system and filled with 0.9% saline containing 100 U/mL heparin. After recovery from anesthesia, the animals were housed individually in special cages with free access to food and tap water until and throughout the experiment. Analgesic treatment with Temgesic (10 μg/kg s.c., application volume 1 mL/kg) was performed in the evening following surgery and in the next morning. Compound administration was in the morning (6-8 AM). Blood samples were collected at various time points from the femoral artery catheter into Eppendorf tubes coated with sodium EDTA. Blood samples were immediately frozen at –20 °C until final processing (maximum storage was 8 days). Intravenous and oral dosing was performed in the same animals after a 48 h wash-out interval between the single dose applications. The test substance was administered intravenously as a solution in 1-methyl-2-pyrrolidone and polyethylene glycol 200 (30:70, v/v) at a dose of 1 mg/kg and orally as a homogenous aqueous suspension in Tween 80 and carboxymethyl cellulose sodium 0.5/0.5/99 (w/w) at a dose of 3 mg/kg [1].

别名	CDZ173
分子量	450.46
分子式	C21H25F3N6O2
CAS No.	1354690-24-6

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: 10 mg/mL

DMSO: 85 mg/mL

H2O: Insoluble

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Hoegenauer K, et al. Discovery of CDZ173 (Leniolisib), Representing a Structurally Novel Class of PI3K Delta-Selective Inhibitors. ACS Med Chem Lett. 2017 Aug 25;8(9):975-980. 2. Rao V, et al. Effective 'Activated PI3Kd Syndrome' -targeted therapy with PI3Kd inhibitor leniolisib. The New England journal of medicine: NEJM. ISSN 20028-4793; 1533-4406

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Leniolisib 1354690-24-6 DNA Damage/DNA Repair PI3K/Akt/mTOR signaling PI3K DNA-PK inhibit CDZ 173 Inhibitor Phosphoinositide 3-kinase CDZ-173 CDZ173 inhibitor

我们的所有产品和服务仅用于科学研究，不能被用于人体，我们也不向个人提供产品和服务。

沪公网安备 31010602006700号

陶术

生物

TargetMol^®中国区唯一合作伙伴

点击进入陶术生物官网

联系我们

电话：

400-820-0310

邮箱：

service@tsbiochem.com

QQ：

2881945090（终端用户）

2885109491（经销商）

经销：

终端：

地址：

上海市静安区江场三路238号8楼

Leniolisib

存储

溶解度

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords